scholarly journals Synthesis, characterization and pharmacological evaluation of substituted phenoxy acetamide derivatives

2015 ◽  
Vol 69 (4) ◽  
pp. 405-415 ◽  
Author(s):  
Priyanka Rani ◽  
Dilip Pal ◽  
Rahul Hegde ◽  
Syed Hashim
Keyword(s):  
Analgesic Activity ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
The Novel ◽  
Standard Drug ◽  
Antipyretic Activity ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

A novel series of 2-(substituted phenoxy)-N-(1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl)acetamide and N-(2-bromocyclohexyl)-2-(substituted phenoxy)acetamide derivatives having cyclohexyl nucleus as common in both types were synthesized and assessed for their anti-inflammatory activity by a carrageenan induced rat paw oedema method, analgesic activity by Eddy?s hot plate method and antipyretic activity by brewer?s yeast induced pyrexia method. All the novel derivatives have been synthesized by the reaction of camphor and similar ketone having cyclohexane nucleus (e.g. 2-bromocyclohexanone) with ammonium carbonate and formic acid resulting in the formation of aromatic amines (1a-b). These amines on further chloroacetylation with chloroacetylchloride give compounds (2a-b). Compounds (2a-b) are converted to 2-(substituted phenoxy)-N-(1,7,7-trimethylbicyclo[2.2.1]heptan-2-yl) acetamide and N-(2-bromocyclohexyl)-2-(substituted phenoxy)acetamide derivatives on treatment with substituted phenol. Among the series 3a-f, 3i, 3k, 3l compounds showed significant anti-inflammatory activity as compared to the standard drug diclofenac sodium and also compound 3a-f, 3h, 3j, 3k exhibit significant analgesic activity as compared to the standard drug. Compounds 3a-f and 3k showed antipyretic activity nearly to the standard drug indomethacin. Compounds 3a-f and 3k possess anti-inflammatory, analgesic and antipyretic activities near to the standard.

scholarly journals Evaluation of analgesic and anti-inflammatory activity of Levocetirizine in albino rats

2019 ◽  
Vol 8 (8) ◽  
pp. 1805
Author(s):  
Dipti R. Sonawane ◽  
Jugalkishor B. Jaju ◽  
Ganesh R. Pawar ◽  
Punam A. Gosavi
Keyword(s):  
Analgesic Activity ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Hot Plate ◽  
Plate Method ◽  
Standard Drug ◽  
Group I ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Tail Clip

Background: Levocetirizine, the R-enantiomer of Cetirizine has pharmacokinetically and pharmacodynamically favourable characteristics, with rapid onset of action, high bioavailability, high affinity for and occupancy of the H1-receptor, limited distribution, minimal hepatic metabolism together with minimal side effects. Non-steroidal anti-inflammatory drugs (NSAIDs) have been used for many years for analgesic, anti-inflammatory, and more recently in the case of aspirin, antithrombotic purposes. Because of the significant side effect profiles of steroidal and NSAID medications, there is a greater interest in newer compounds such as antihistaminic drugs. This article will consider the potential or otherwise of the reported analgesic and anti-inflammatory effects of levocetirizine to enhance its effectiveness in the treatment of allergic disease with pain.Methods: Albino Wistar rats of either sex weighing 150-250 grams were used. For both Analgesic activity and Anti-inflammatory activity, 4 groups consisting of 6 animals per group were used. Group I: Control: 1% Gum acacia. 2ml/kg, Group II: Standard drug: Diclofenac sodium 4.5mg/kg; Group III: Test Drug 1: Levocetirizine 1mg/kg; Group IV: Test Drugs 2: Levocetirizine 1mg/kg+Diclofenac sodium 4.5mg/kg. Drugs were administered orally. For analgesic activity, Tail clip method and Hot plate method was used. For acute anti-inflammatory activity Carrageenan induced rat paw oedema method was used.Results: Levocetirizine, is found to have significant analgesic activity in rats (1 mg/kg dose) alone and in combination with Diclofenac Sodium in Haffner’s Tail Clip method and Eddy’s Hot Plate Method. Levocetirizine also has got prominent anti-inflammatory activity in acute models evidenced by percentage inhibition of acute rat paw oedema.Conclusions: Levocetirizine possess analgesic and acute anti-inflammatory activity alone and in combination with Diclofenac sodium.

scholarly journals ANTI-INFLAMMATORY ACTIVITY OF METHANOLIC EXTRACT OF PLANT SIDA CORDATA IN CARRAGEENAN-INDUCED PAW EDEMA IN RATS

2021 ◽  
Vol 10 (2) ◽  
pp. 53-55
Author(s):  
Prajakta P Shinde ◽  
Shahu D Khule ◽  
Sneha Sonawane ◽  
Suvarna Shelke
Keyword(s):  
Methanolic Extract ◽  
White Blood Cells ◽  
Inflammatory Activity ◽  
Clinical Practices ◽  
Standard Drug ◽  
Paw Oedema ◽  
Ancient Times ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

Since ancient times in India several medicinal plants are in use for clinical practices. Inflammation is a process through which the body's white blood cells and the things they make protect body from infection from outside invaders, such as bacteria and viruses. Currently many of the plant’s species have been reported effective as an Anti-inflammatory, but only a few of them have been investigated. Currently many drugs are available to control the inflammation but has several adverse effects. The plant Sida Cordata was reported to have several activities such as Antioxidant, Analgesic, Antidepressant, Antihyperglycemic, Hepatoprotective Antibacterial, Antitumor, Antifungal, Antiulcer, Antitussive, Anti-inflammatory, Anti-malarial, in ayurvedic system of medicine. This study was undertaken to investigate the anti-inflammatory activity of Methanolic extract of Sida Cordata. The methanolic extract of Sida Cordata used for treatment of Carrageenan-induced Rat paw Oedema model with the predefined dose as reported. The experimental groups with higher dose of methanolic extract (200 mg/kg) exhibited a significant anti-inflammatory effect after 2 hr. (p<0.01); based on the observation, the activity was favorable, which is nearly equal to that of the standard drug Indomethacin (10 mg/kg). The methanol extract (200 mg/kg) shows the maximum percentage of inhibition of inflammation 27.06 %. The standard drug indomethacin shows 33 % inhibition.

scholarly journals Anti-Inflammatory Activity of Pleurotus ostreatus, a Culinary Medicinal Mushroom, in Wistar Rats

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
W. J. A. Banukie N. Jayasuriya ◽  
Shiroma M. Handunnetti ◽  
Chandanie A. Wanigatunge ◽  
Gita H. Fernando ◽  
D. Thusitha U. Abeytunga ◽  
...  
Keyword(s):  
Pleurotus Ostreatus ◽  
Inflammatory Activity ◽  
No Production ◽  
Protective Effects ◽  
Paw Oedema ◽  
Freeze Dried ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

Context. Pleurotus ostreatus (P.o) is a culinary mushroom which is commonly called as “oyster mushroom” belonging to the Basidiomycetous fungi of the order Agaricales and family Pleurotaceae. Objectives. The present study investigates the anti-inflammatory potential of P.o and the underlying mechanisms of activity. Materials and Methods. Anti-inflammatory activity was evaluated using suspensions of freeze-dried and powdered (SFDP) P.o and acetone extract (AE) of P.o in normal and alloxan-induced diabetic rats using the carrageenan-induced rat paw oedema model. The mechanisms by which P.o is mediating the anti-inflammatory activity were studied using in vivo and in vitro assays. Results. At doses of 500–1000 mg/kg, the SFDP of P.o showed long-lasting activity at both early and late phases of carrageenan-induced rat paw oedema. The dose of 750 mg/kg showed the most potent inhibitory activity (92% inhibition) in healthy rats. The AE of P.o showed maximum inhibition of oedema of 87%. P.o exerted protective effects on the inflammatory pathologies in rats with diabetes. The possible mechanisms by which P.o mediates the anti-inflammatory activity were antihistamine activity (52.1%), inhibition of cell migration to the site of inflammation (45.4%), in vitro membrane stabilizing activity (52.6%), and inhibition of nitric oxide (NO) production (91.2%) (P<0.05). Dose-dependent inhibition of NO production was seen with in vitro treatment of rat peritoneal cells with AE of P.o (r = 0.95; P<0.05). Discussion and Conclusion. The promising activity of culinary mushroom P.o against inflammation suggests its potential application as a functional food during inflammatory conditions.

scholarly journals Anti-Inflammatory Activity of Hydroxytriazenes and their Vanadium Complexes

2008 ◽  
Vol 5 (s2) ◽  
pp. 1144-1148 ◽  
Author(s):  
Kalpana Singh ◽  
Peeyush Patel ◽  
A. K. Goswami
Keyword(s):  
Body Weight ◽  
Metal Complexes ◽  
Diclofenac Sodium ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
Vanadium Complexes ◽  
Standard Drug ◽  
Standard Methods ◽  
Paw Oedema ◽  
Anti Inflammatory

The anti-inflammatory activity of hydroxytriazenes as well as their vanadium complexes has been studied using carrageenan induced hind paw oedema method in albino rats (Wister strain). Hydroxytriazenesviz., 3-hydroxy-1,3-diphenyltriazene(HT-1), 3-hydroxy-3-phenyl-1-(4-sulfonamido)phenyl triazene(HT-2), 3-hydroxy-3-p-chlorophenyl-1-(4-sulfonamido) phenyltriazene(HT-3), 3-hydroxy-3-m-chlorophenyl-1-(4-sulfonamido)phenyltriazene(HT-4)(HT-4) and their respective vanadium complexes C-1, C-2, C-3 and C-4 have been synthesized using standard methods, purified, characterized and used for studying their anti-inflammatory activities. The hind paw oedema was produced by subplanter injection of carrageenan and the paw volume was measured plethysmographically after 0.5, 1, 2, 3 and 5 h. The animals were givenHT-1, HT-2, HT-3andHT-4and also vanadium complexes C-1, C-2, C-3 and C-4 dissolved inDMSO(at dose 5 mg/Kg body weight). Diclofenac sodium (5 mg/kg) was used as a standard drug. The standard drug shows maximum inibition up to 1h as 81.73% which goes on increasing up to 3h (88.94%) but further reduces to 74.93% at the end of 5 h. The test compounds i.e. both ligands as well as their metal complexes show maximum percent inhibition only up to 1h. after which the efficacy reduces. Thus it can be said that both ligands as well as their vanadium complexes show very significant anti-inflammatory activity up to 1h which is comparable to standard drug.

Analgesic and anti-inflammatory activity of Tectona grandis Linn. stem extract

2015 ◽  
Vol 26 (5) ◽  
Author(s):  
Sapna P. Giri ◽  
Sushilkumar B. Varma
Keyword(s):  
Analgesic Activity ◽  
Radiant Heat ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
Standard Drug ◽  
Writhing Test ◽  
Paw Oedema ◽  
Stem Extract ◽  
Heat Method ◽  
Anti Inflammatory

AbstractThe objective of this work was to study the analgesic and anti-inflammatory activity ofHealthy albino rats (150–200 g) and mice (25–50 g) were arranged and divided into five groups. Group 1 received distilled water and served as control, groups 2, 3, 4 were treated with TG stem extract (100, 200, 400 mg/kg) and group 5 received standard drug. For analgesic activity, the radiant heat method and writhing test were used, and for anti-inflammatory activity, the paw oedema model and granuloma pouch method were used. Statistical analysis was done by one-way analysis of variance followed by the t-test.In the radiant heat method, there was a dose-dependent increase in reaction time in TG stem extract (100, 200, 400 mg/kg) and standard drug (buprenorphine). In the writhing test, TG stem extract (200, 400 mg/kg) and aspirin decreased the number of writhes which was significant (p<0.01, p<0.001) as compared to controls. The percentage protection was 8.88%, 15.55%, 22.22% and 35.55% in groups 2, 3, 4 and 5, respectively. In the rat paw oedema test, TG stem extract (200, 400 mg/kg) and aspirin showed 20%, 40% and 54% inhibition of oedema which was statistically significant (p<0.05, p<0.01, p<0.001), respectively, as compared to control at the end of 4 h. In the granuloma pouch method, TG stem extract (100, 200, 400 mg/kg) and aspirin showed 13.33%, 22.22%, 33.33% and 66.66% inhibition of granuloma, respectively, which was significant (p<0.05, p<0.01, p<0.001).TG stem extract possesses significant anti-inflammatory and analgesic activity.

scholarly journals Anti-inflammatory and Anti-arthritic Activities ofMerremia tridentate(L.) Hall. f.

2009 ◽  
Vol 6 (4) ◽  
pp. 943-948 ◽  
Author(s):  
M. Kamalutheen ◽  
S. Gopalakrishnan ◽  
T. Syed Ismail
Keyword(s):  
Ethanol Extract ◽  
Albino Rats ◽  
Standard Drug ◽  
Arthritis Model ◽  
Paw Oedema ◽  
Dependent Activity ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Dose Dependent ◽  
Rat Paw Oedema

The various extracts ofMerremia tridentatewere investigated for its anti-inflammatory and anti-arthritic activities in male albino rats. The anti-inflammatory activity was carried out using carrageenan-induced rat paw oedema model and the anti-arthritic activity was carried out using complete Freund’s adjuvant induced arthritis model. Indomethacin (10 mg/kg bw) was used as a standard drug. The ethanol extract ofM. tridentateexhibited significant dose dependent activity in acute inflammation and the doses of 100 mg/kg bw and 200 mg/kg bw produced 38.3% and 42.8% inhibition respectively after 3 h as compared with that of the standard drug which showed 48.5% inhibition. In arthritis model, the doses of 100 mg/kg bw and 200 mg/kg bw of the ethanol extract produced 49.0% and 51.7% inhibition respectively after 19 days when compared with that of the standard drug (55.5%). Both doses of the ethanol extract ofM. tridentateexhibit significant anti-inflammatory and anti-arthritic activities.

scholarly journals Screening for anti-inflammatory activity of extract and fractions of Morinda lucida stem bark and detection of bioactive secondary metabolite

2021 ◽  
Vol 16 (1) ◽  
pp. 031-039
Author(s):  
Chukwubuikem C. Okolo ◽  
Nancy A. Mbachu ◽  
Ogechi O. Anyanwu ◽  
Kenneth G. Ngwoke ◽  
Festus B.C. Okoye
Keyword(s):  
Stem Bark ◽  
Positive Control ◽  
Inflammatory Activity ◽  
Paw Oedema ◽  
Dependent Inhibition ◽  
Egg Albumen ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Ear Oedema ◽  
Rat Paw Oedema

Morinda lucida Benth (Rubiaceae) is a versatile plant used in traditional medicine for the treatment of a variety of ailments and the claims of its efficacy are particularly remarkable in the treatment of infections and immuno-inflammatory disorders. This study evaluates the anti-inflammatory properties of methanolic stem bark extract and fractions of M. lucida and also identifies the phytochemicals responsible for its anti-inflammatory activity. The crude extract was subjected to liquid- liquid partitioning successively with n- hexane, ethylacetate, butanol and water. High performance liquid chromatography (HPLC) of the four fractions and Vacuum Liquid Chromatography fraction (VLC) of the promising fraction was evaluated. The effect of the fractions on egg albumen induced rat paw oedema were also evaluated. Anti-inflammatory activity of the fractions was further screened using xylene induce ear oedema models and human red blood cell membrane stabilization test. Ulcerogenic test on the normal stomach mucosa was also evaluated. The result of the egg albumen induced rat paw oedema showed that the butanol fractions maximally inhibited egg albumen induced effect at 400 mg/kg (70%) and 200mg/kg (67.5%) after 180 minutes compared to the positive control, ibuprofen (20mg/kg) with 100% inhibition after 180 minutes. The result of the xylene induced ear oedema showed that the inhibition produced by 100 µg/ear of the Butanol fraction (BF) was 56.67 % and was greater than inhibition produced by 200 µg/ear of ibuprofen (38.89 %). HPLC analysis of the fractions revealed the following phytocompounds; Cytreo- a-pyrone, Cytosporin- J and Waol A. Ulcerogenic test was negative at the doses of 200 mg/kg and 400 mg/kg of the fractions when compare with the indomethacin (positive control) at dose of 50 mg/kg. Human red blood cell membrane stabilization assay showed that BF-VLC 2 (Dichloromethane: methanol (8:2) VLC of Butanol fraction) exhibited concentration dependent inhibition of heat-induced haemolysis while other extract showed a non- concentration dependent inhibition of haemolysis when compared to the standard, ibuprofen. These findings suggest that the stem bark of M. lucida possess promising anti-inflammatory phytocompounds which justify its use in ethno-medicine.

scholarly journals Anti-inflammatory activity of Syzygium cumini leaf against experimentally induced acute and chronic inflammations in rodents

2011 ◽  
Vol 1 (1) ◽  
pp. 6 ◽  
Author(s):  
Anirban Roy ◽  
Sanjib Bhattacharya ◽  
Jitendra N. Pandey ◽  
Moulisha Biswas
Keyword(s):  
Inflammatory Activity ◽  
Dependent Manner ◽  
Syzygium Cumini ◽  
Large Size ◽  
Paw Oedema ◽  
Chronic Models ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Dose Dependent ◽  
Rat Paw Oedema

<p><em>Syzygium cumini<strong> </strong></em>(L.) Skeels (Myrtaceae), commonly known as <em>Jam </em>in Bengali, <em>Jamun</em> in Hindi and <em>Black Plum</em> or <em>Black Berry</em> in English, is a large size evergreen tree indigenous to India and is cultivated for its fruits. In the present study, the methanol extract of leaves from <em>S. cumini </em>(MESC) was evaluated for anti-inflammatory activity in experimental acute (carrageenan, histamine and serotonin induced rat paw oedema) and chronic models (cotton pellet induced rat granuloma). In all models, the MESC (100 and 200 mg/kg body wt. p.o.) exhibited significant anti-inflammatory activity (<em>p &lt; 0.001</em>) in a dose dependent manner. These findings revealed that the <em>S. cumini </em>leaf had remarkable acute and chronic anti-inflammatory actions in the tested rodent models.</p>

SYNTHESIS, BIOLOGICAL EVALUATION, QSAR AND DOCKING STUDIES OF 2-AMINO-5-(SUBSTITUTED)PHENYL-1,3,4-THIADIAZOLES

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (09) ◽  
pp. 5-12
Author(s):  
S. S Mahajan ◽  
◽  
A. D. Gaitonde
Keyword(s):  
Analgesic Activity ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Qsar Studies ◽  
Paw Oedema ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Rat Paw ◽  
Rat Paw Oedema

Ten compounds from the series of 2-amino-5-(substituted)phenyl-1,3,4-thiadiazoles were synthesized and evaluated for anti-inflammatory and analgesic activities. Their structures were characterized by infrared spectroscopy and confirmed by 1H NMR spectroscopy. Anti-inflammatory activity was carried out by carrageenan-induced rat paw oedema method using indomethacin as standard. Analgesic activity was performed by acetic-acid induced writhing method in mice using aspirin as standard. The QSAR studies were performed for the analgesic activity using the software ‘Strike’ from Schrodinger. Docking studies were carried out for COX-2 inhibition using the software ‘Glide’ from Schrodinger. The compounds were obtained in good yields and possessed good anti-inflammatory and analgesic activities. Various physicochemical parameters, contributing towards analgesic activity were identified from the QSAR studies. The Glide Scores were more or less correlated with the anti-inflammatory and analgesic activities of compounds.

scholarly journals Synthesis of N-((2-Substituted Phenyl)-4, 5-Diphenyl-1H-Imidazol1yl)(Phenyl)Methyl) substituted amine derivatives, spectral characterization and their pharmacological evaluation

2011 ◽  
Vol 1 (5) ◽  
pp. 184-190 ◽  
Keyword(s):  
Aromatic Aldehyde ◽  
Analgesic Activity ◽  
Elemental Analysis ◽  
Spectral Characterization ◽  
Hot Plate ◽  
Pharmacological Evaluation ◽  
Paw Oedema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Rat Paw Oedema

A series of N-((2-substituted phenyl) -4,5-diphenyl-1H-imidazol-1yl)(phenyl)methyl) substituted amine derivatives TPI (I-V) were synthesized by 2-substituted 4,5-diphenyl imidazole derivatives starting from benzyl and aromatic aldehyde. All these compounds were characterized by IR, 1HNMR, mass and elemental analysis. The newly synthesized compounds were screened for analgesic and anti-inflammatory activities by hot plate and carrageenan induced rat paw oedema methods. Compounds TPI-IV and TPI-V have showed potent anti-inflammatory activity and compounds TPI-III, TPI-IV and TPI-V showed good analgesic activity

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